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HG-12-6 is a Novel type II inhibitor of IRAK4, showing preferential binding to unphosphorylated inactive IRAK4. | [Uses]
HG-12-6 is a type II inhibitor of IRAK4. HG-12-6 shows preferential binding to unphosphorylated inactive IRAK4 with an IC50 of 165 nM. HG-12-6 can modulate IRAK4 activity in autoimmunity and inflammation[1]. | [IC 50]
IRAK4: 165 nM (IC50, Unphosphorylated inactive IRAK4 ); IRAK4: 2876 nM (IC50, Phosphorylated active IRAK4 ) | [References]
[1] Wang L, et al. Conformational flexibility and inhibitor binding to unphosphorylated interleukin-1 receptor-associated kinase 4 (IRAK4). J Biol Chem. 2019 Mar 22;294(12):4511-4519. DOI:10.1074/jbc.RA118.005428 |
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